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Chemical Structure| 2089148-72-9 Chemical Structure| 2089148-72-9

Structure of A-395
CAS No.: 2089148-72-9

Chemical Structure| 2089148-72-9

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A-395 is a antagonist of Polycomb repressive complex 2 (PRC2) protein–protein interactions that potently inhibits the trimeric PRC2 complex (EZH2–EED–SUZ12) with an IC50 of 18 nM.

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Product Details of A-395

CAS No. :2089148-72-9
Formula : C26H35FN4O2S
M.W : 486.65
SMILES Code : CN(C)[C@H]([C@@H](C1=CC=C(N2CCN(S(=O)(C)=O)CC2)C=C1)C3)CN3C(CC4)C5=C4C=CC=C5F
MDL No. :MFCD31563589

Safety of A-395

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of A-395

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human umbilical vein endothelial cells (HUVECs) 5 μM 24 h Inhibition of PRC2 complex activity, increased ITGA4 expression, improved endothelial cell migration and adhesion Mol Ther Nucleic Acids. 2024 Apr 6;35(2):102173
JLat6.3 cells 10 μM 72 h Evaluate the effect of A-395 on HIV latency reversal, results showed A-395 alone or in combination with SAHA did not significantly increase GFP expression. ACS Infect Dis. 2020 Jul 10;6(7):1719-1733
JLatA2 cells 10 μM 72 h Evaluate the effect of A-395 on HIV latency reversal, results showed A-395 alone increased GFP expression by 2-fold, and when combined with SAHA, increased to 3-4-fold. ACS Infect Dis. 2020 Jul 10;6(7):1719-1733
2D10 cells 10 μM 72 h Evaluate the effect of A-395 on HIV latency reversal, results showed A-395 alone increased GFP expression by 1.9-fold, and when combined with SAHA, increased to 17.3-fold. ACS Infect Dis. 2020 Jul 10;6(7):1719-1733

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Hindlimb ischemia model Intraperitoneal injection 10 mg/kg Twice per week for 3 weeks Inhibition of EZH2 enzymatic activity, increased ITGA4 expression, promoted arteriogenesis Mol Ther Nucleic Acids. 2024 Apr 6;35(2):102173

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02876757 - Completed - -
NCT02876757 - Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.21mL

10.27mL

2.05mL

1.03mL

20.55mL

4.11mL

2.05mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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